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Literature summary for 3.5.1.98 extracted from

  • Schuetz, A.; Min, J.; Allali-Hassani, A.; Schapira, M.; Shuen, M.; Loppnau, P.; Mazitschek, R.; Kwiatkowski, N.P.; Lewis, T.A.; Maglathin, R.L.; McLean, T.H.; Bochkarev, A.; Plotnikov, A.N.; Vedadi, M.; Arrowsmith, C.H.
    Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity (2008), J. Biol. Chem., 283, 11355-11363.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.1.98

Cloned(Commentary)

Cloned (Comment) Organism
residues 483 to 903 of isoform 1 of chHDAC7 are cloned into a modified pET28a vector for expression in Escherichia coli BL21DE3 Codon Plus RIL cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
the crystal structures of the catalytic domain of HDAC7 and its complexes with suberoylanilide hydroxamic acid and trichostatin A are solved Homo sapiens

Protein Variants

Protein Variants Comment Organism
H843A mutant, constructed to assess the role of the active site His-843 Homo sapiens
H843F mutant, constructed to assess the role of the active site His-843 Homo sapiens
H843Y mutant, constructed to assess the role of the active site His-843 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
-
 Homo sapiens
LAQ824
-
 Homo sapiens
LBH589
-
 Homo sapiens
oxamflatin
-
 Homo sapiens
suberoylanilide hydroxamic acid SAHA Homo sapiens
trichostatin A TSA Homo sapiens
tubacin
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.013
-
 Fluor de Lys HDAC substrate mutant H843Y Homo sapiens
0.016
-
 Fluor de Lys HDAC substrate mutant H843A Homo sapiens
0.016
-
 Fluor de Lys HDAC substrate mutant H843F Homo sapiens
0.017
-
 Fluor de Lys HDAC substrate wild type enzyme Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens HDACs catalyze the deacetylation of lysine residues in the N-terminal tails of core histones, in addition non-histone proteins may also serve as substrates ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q8WUI4
-
-

Purification (Commentary)

Purification (Comment) Organism
by affinity chromatography on a 5-ml HiTrap Chelating column charged with Ni2+ and by anion exchange chromatography on a Source 30Q column Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Fluor de Lys HDAC substrate + H2O commercially available kit Homo sapiens ?
-
 ?
additional information HDACs catalyze the deacetylation of lysine residues in the N-terminal tails of core histones, in addition non-histone proteins may also serve as substrates Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
class IIa histone deacetylase
-
 Homo sapiens
HDAC7
-
 Homo sapiens
histone deacetylase 7
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0002
-
 Fluor de Lys HDAC substrate wild type enzyme Homo sapiens
0.017
-
 Fluor de Lys HDAC substrate mutant H843F Homo sapiens
0.018
-
 Fluor de Lys HDAC substrate mutant H843A Homo sapiens
1.1
-
 Fluor de Lys HDAC substrate mutant H843Y Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
 mutant H843Y Homo sapiens (2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
0.00004
-
 mutant H843Y Homo sapiens trichostatin A
0.00013
-
 mutant H843Y Homo sapiens LBH589
0.0003
-
 mutant H843Y Homo sapiens suberoylanilide hydroxamic acid
0.0003
-
 wild type Homo sapiens trichostatin A
0.0008
-
 mutant H843Y Homo sapiens tubacin
0.0026
-
 mutant H843Y Homo sapiens oxamflatin
0.0036
-
 mutant H843Y Homo sapiens LAQ824
0.0043
-
 wild type Homo sapiens (2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
0.0154
-
 wild type Homo sapiens LBH589
0.098
-
 wild type Homo sapiens oxamflatin
0.113
-
 wild type Homo sapiens suberoylanilide hydroxamic acid
0.225
-
 wild type Homo sapiens tubacin
0.553
-
 wild type Homo sapiens LAQ824